glutamate receptor

Kynurenic acid (Quinurenic acid) is an endogenous tryptophan active metabolite, a triple antagonist of NMDA, glutamate, α7 nicotinic acetylcholine receptor, and an agonist of GPR35 CXCR8 with neuroprotective and anticonvulsant properties. It has neuroprotective and anticonvulsant properties and can be used to study neurodegeneration and metabolism-related diseases.

In the CNS, Kainic acid is an effective agonist at excitatory amino acid receptor subtypes.

7-Chlorokynurenic acid (7-chloro-4-hydroxy-2-carboxyquinoline) is an effecitve and selective antagonist of NMDA receptor with IC50 of 0.56 μM for the glycine B coagonist site. 7-Chlorokynurenic acid inhibits the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM and shows antinociceptive actions after neuraxial delivery.

N-Methyl-D-aspartic acid is an amino acid that, as the D-isomer, is the defining agonist for the NMDA (N-Methyl-D-aspartic acid) receptor subtype of glutamate receptors.

L-Glutamic acid monosodium salt (MSG) (Monosodium glutamate) is an activator of mGlu1 receptor.

O-Phospho-L-serine (Phosphoserine) is the phosphoric acid ester of serine.

D-Serine ((R)-Serine), an endogenous amino acid, is a potent co-agonist at the NMDA glutamate receptor.

1. Linalool (Linalol), a natural compound of the essential oils, has been shown to have antinociceptive, antimicrobial, and anti-inflammatory properties. 2. Linalool was protected against LPS GalN-induced liver injury through induction of antioxidant defense via Nrf2 activating and reduction inflammatory response via NF-κB inhibition. 3. Linalool biosynthesis and accumulation might be involved in plant defense against bacterial and fungal pathogens and be associated with field resistance to citrus canker. 4. Linalool significantly increased the expression of antioxidant enzymes regulated by Nrf-2 and diminished lung tissue levels of several pro-inflammatory cytokines, including tumor necrosis factor α (TNF-α) and interleukin (IL)-6.

Ifenprodil is a selective NMDA receptor (glutamate) antagonist.

1-Aminocyclopropane-1-carboxylic acid (ACC) is an intermediate in the synthesis of ethylene, the plant hormone responsible for biological processes ranging from seed germination to organ senescence. It is a small molecule agonist at the glycine modulatory site of the NMDA receptor (EC50 = 0.7-0.9 μM) in the presence of low levels (1 μM) of glutamate and as a competitive antagonist at the glutamate-binding site on NMDA receptors (EC50 = 81.6 nM) with high levels (10 μM) of glutamate.2 This compound has been reported to protect against neuron cell death in vivo models of ischemia by enabling moderate levels of NMDA receptor activation and attenuating any excess NMDA receptor signaling that may lead to neurotoxicity.

glycine (2-Aminoacetic acid) is a non-essential amino acid. It is found primarily in gelatin and silk fibroin and used therapeutically as a nutrient. It is also a fast inhibitory neurotransmitter.

Hyperforin, a natural product from Hypericum, is commonly used as an antidepressant and also has neurological, inflammatory, antimicrobial, antitumor and antiangiogenic effects. Hyperforin acts as a monoamine reuptake inhibitor (MRI) in vitro, including serotonin, norepinephrine, dopamine, GABA, and glutamate, with an IC 50 of ≈0.1 μg mL. Hyperforin is also capable of inducing the cytochrome P450 enzymes, CYP3A4 and CYP2C9, through binding to and activation of the pregnane X receptor. Hyperforin is capable of activating TRPC6 channels by binding to a specific motif.

Gartanin is an androgen receptor degradation enhancer, it is also a potential neuroprotective agent against glutamate-induced oxidative injury partially through increasing Nrf-2-independed HO-1 and AMPK SIRT1 PGC-1α±signaling pathways.

Aminoadipic acid (DL-2-Aminoadipic acid) (2-aminoadipate) is a metabolite in the principal biochemical pathway of lysine. It is an intermediate in the metabolism (i.e. breakdown or degradation) of lysine and saccharopine. It antagonizes neuroexcitatory activity modulated by the glutamate receptor N-methyl-D-aspartate (NMDA). Aminoadipic acid has also been shown to inhibit the production of kynurenic acid, a broad spectrum excitatory amino acid receptor antagonist, in brain tissue slices.

L-γ-Glutamyl-S-[(4-hydroxyphenyl)methyl] was isolated as the major principle responsible for the inhibition of the in vitro binding of kainic acid to brain glutamate receptors by water extracts of the plant Gastrodia elata.

Sauristolactam inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis and has the potential to inhibit osteoclast differentiation. Sauristolactam, a natural aristolactam isolated from aerial portions of Saururus Chi

Amantadine (1-Aminoadamantane) is an antiviral, is a weak antagonist of the NMDA-type glutamate receptor, increases dopamine release, and blocks dopamine reuptake.

Transcrocetinate disodium (Disodium trans-crocetinate), extracted from saffron (Crocus sativus L.), is a high-affinity antagonist of NMDA receptor.

Ampullosporin A is a peptaibol-type polypeptide isolated from the fungus Sepedonium ampullosporum (HKI-0053), exhibiting neuromodulatory activity. It inhibits hyperactivity induced by the NMDA receptor antagonist MK-801 and ameliorates social behavior abnormalities caused by subchronic ketamine treatment. Ampullosporin A modulates glutamate receptor activity without affecting dopamine D1 and D2 receptors.

Ibotenic acid hydrate ((RS)-Ibotenic acid hydrate) is an excitatory amino acid receptor agonist that primarily exerts its effects by activating glutamate receptors, such as NMDA receptors. Ibotenic acid hydrate can be extracted from the fly agaric mushroom (Amanita muscaria).

γ-L-Glutamyl-L-alanine consists of γ-glutamate and alanine, and is a substrate for CRF21 (γ-glutamyl cyclotransferase, GGCT), a proteolytic breakdown product of larger proteins.γ-L-Glutamyl-L-alanine is a positive regulator of calcium-sensitive receptor (CaR) function.